Bergenin review
February 2 2017 by Ray Sahelian, M.D.
Bergenin monohydrate is an isocumeric compound that is found in several herbs. It is a C-glycoside of 4-O-methyl gallic acid. Bergenin may have potential to treat cardiac arrhythmias.
Review article
Fitoterapia. 2015. Diversity, pharmacology and synthesis of bergenin and its
derivatives: Potential materials for therapeutic usages. Bergenin, a natural
secondary metabolite, has been isolated from different parts of a number of
plants. It is one of active ingredients in herbal and Ayurvedic formulations. It
exhibits antiviral, antifungal, antitussive, antiplasmodial, antiinflammatory,
antihepatotoxic, antiarrhythmic, antitumor, antiulcerogenic, antidiabetic and
wound healing properties.
Benefit for heart rhythm problems
Bergenin is the antiarrhythmic principle
of Fluggea virosa.
Planta Med. 2002.
Bergenin was isolated from the aerial parts of Fluggea virosa. Anti-arrhythmic effects of bergenin were investigated.
It showed distinct
therapeutic effects on BaCl2-induced arrhythmias in rats. At
concentrations of 0.4 mg/kg and 0.8 mg/kg bergenin significantly countered
arrhythmias induced by ligation and reperfusion of the coronary artery. At
0.8 mg/kg, bergenin elevated the atria fibrillation threshold in rabbits
from 1.3 mV to 1.9 mV. Our results suggest that bergenin has good
potential to treat cardiac arrhythmias.
Some plants that have bergenin
Ardisia colorata fruits have ardisiphenols, bergenin, a bergenin derivative
demethoxybergenin, alkylresorcinols, embelin, myricetin, quercetin, norbergenin,
kaempferol, quercetin-3-O-beta-D-glucopyranoside and gallic acid.
Ardisia japonica has about 50 to 60 percent bergenin. The content of bergenin in
Ardisia pusilla and Ardisia japonica is similar.
Astilbe chinensis has bergenin
Astilbe thunbergii
Bergenia
crassifolia
Bergenia ligulata herb has bergenin and gallic acid.
Bergenia stracheyi
Flueggea virosa leaves have a good amount of bergenin.
Mallotus japonicus has a good amount of bergenin. Norbergenin, which is the O-demethyl
derivative of bergenin, the main component of Mallotus japonicus, has moderate
antioxidant activity.
Mallotus roxburghianus is used in the traditional medicine in North-Eastern
India and contains bergenin.
Sacoglottis gabonensis bark has bergenin.
Antioxidant properties
Antioxidant activity of bergenin: a phytoconstituent
isolated from the bark of Sacoglottis uchi Huber (Humireaceae).
Org Biomol Chem. 2008; De Abreu HA, Aparecida Dos S Lago I, Souza GP,
Piló-Veloso D, de C Alcântara AF. Departamento de Química,Universidade Federal de Minas Gerais, Belo Horizonte, MG, Brazil.
Bergenin was isolated from Sacoglottis uchi, a species of vegetable found in the
Amazon region and popularly used for the treatment of several hepatic problems.
This phytoconstituent has been used as an oriental folk medicine for the
treatment of many diseases and shows liver protecting properties. We confirmed
the antioxidant properties of bergenin.
Bergenin research studies
Protective effects of bergenin, the major constituent of Mallotus japonicus,
on D-galactosamine-intoxicated rat hepatocytes.
J Ethnopharmacol. 2000.
This study was designed to investigate the effects of bergenin against D-galactosamine-induced
injury in primary cultured rat hepatocytes. Bergenin decreased the
release of glutamic pyruvic transaminase and sorbitol dehydrogenase into
hepatocyte medium incubated for galactosamine. The present
results suggest that bergenin show liver protective effects against
galactosamine-intoxicated rat hepatocytes by inhibiting the release of glutamic
pyruvic transaminase and sorbitol dehydrogenase as well as by increasing RNA
synthesis.
Antihepatotoxic activity of bergenin, the major constituent of Mallotus
japonicus, on carbon tetrachloride-intoxicated hepatocytes.
J Ethnopharmacol. 2000.
To determine the antihepatotoxic activity of bergenin from Mallotus japonicus,
carbon tetrachloride (CCl4)-induced cytotoxicity in primary cultured rat
hepatocytes has been adopted as an assay system. Bergenin significantly reduced
the activities of glutamic pyruvic transaminase and sorbitol dehydrogenase
released from the CCl4-intoxicated liver cells. The antihepatotoxicity of
bergenin was also evidenced by elevating the activities of glutathione S-transferase
and glutathione reductase, and content of glutathione in the CCl4-intoxicated
hepatocytes. From these results, it is assumed that bergenin exerted
antihepatotoxicity against CCl4-induced cytotoxicity through
glutathione-mediated detoxification as well as free radical suppressing
activity.
How to easily replace the independent atom model - the
example of bergenin, a potential anti-HIV agent of traditional Asian medicine.
Acta Crystallogr B. 2009; Dittrich B, Weber M, Kalinowski R, Grabowsky
S, Hübschle CB, Luger P. Institut für Anorganische Chemie, Georg-August-Universität
Göttingen, Tammanstrasse 4, Göttingen, Germany.
Bergenin, which has been isolated from a variety of tropical plants, has several
pharmacological applications in traditional Asian medicine. Its electron-density
distribution was obtained from a room-temperature low-resolution X-ray data set
measured with point detection making use of multipole populations from the
invariom library. Two refinement models were considered. In a first step,
positional parameters and ADPs were refined with fixed library multipoles (model
E1). This model was suitable to be input into a second refinement of multipoles
(model E2), which converged smoothly although based on Cu Kalpha
room-temperature data. Quantitative results of a topological analysis of the
electron density from both models were compared with Hartree-Fock and
density-functional calculations. With respect to the independent atom model (IAM)
more information can be extracted from invariom modelling, including the
electrostatic potential and hydrogen-bond energies, which are highly useful,
especially for biologically active compounds. The reliability of the applied
invariom formalism was assessed by a comparison of bond-topological properties
of sucrose, for which high-resolution multipole and invariom densities were
available. Since a conventional X-ray diffraction experiment using basic
equipment was combined with the easy-to-use invariom formalism, the procedure
described here for bergenin illustrates how it can be routinely applied in
pharmacological research.
Absorption of bergenin
Kinetics study on intestinal absorption of bergenin in
rats.
Sichuan Da Xue Xue Bao Yi Xue Ban. 2007. Key Laboratory of Drug
Targeting of Ministry of Education, West China School of Pharmacy, Sichuan
University, Chengdu, China.
To study the kinetics of intestine absorption of bergenin in rats. The intestine
absorption of bergenin in the rats was determined by in situ perfusion. The HPLC
were used to determine the concentration of bergenin in the perfusate and the
plasma. The concentrations of bergenin in various sites of the intestine and the
pH values were studied. The absorption of bergenin exhibited linear kinetics. The absorption varied in the duodenum,
jejunum, ileum and colon. In the range of pH 5.4-7.8, with the increasing of
pH value, the Ka of bergenin decreased. Bergenin is absorbed by the entire
intestine, but with limited amount. The absorption of the drug is a first-order
process with the passive diffusion mechanism.
Constituents of Ardisia japonica and their in vitro anti-HIV activity
J Nat Prod. 1996.
As part of our screening of anti-AIDS agents from medicinal plants, the MeOH
extract of the aerial parts of Ardisia japonica was tested, and it showed
moderate in vitro anti-HIV activity. Reexamination to identify the compounds
responsible for the anti-HIV activity revealed several known compounds and a new
triterpenoid saponin. All of the isolated compounds were tested and, although
none of the triterpenoid saponins was active, bergenin and norbergenin showed
weak anti-HIV activity.
Studies on the chemical constituents of Ardisia crenata Sims
Zhongguo Zhong Yao Za Zhi. 1989.
A new bergenin derivative isolated from the root of Ardisia crenata was
determined to be 11-o-syringylbergenin by spectral methods. Other compounds were
identified as spinasterol, series fatty acids, beta-sitosterol-beta-D-glucoside,
norbergenin and sucrose respectively. The last three were obtained for the first
time from the genus of Ardisia.